Signal Transduction - GPCR Flashcards

1
Q

What receptor is shown?

A

GPCR

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2
Q

Can the effector of a GPCR be an ion channel?

A

Yes

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3
Q

Where does the receptor exist in a GPCR?

A

Plasma membrane

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4
Q

What 2 receptors can the G protein activate?

A

Enzyme or ion channel

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5
Q

What are seconds messengers?

A

Transfer a signal from the membrane to the rest of the cell

After (receptor activation)

soluble products

intracellular site of action

amplify the response

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6
Q

When the ligand activates the GPCR, is the signal continuous?

A

Yes

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7
Q

What is the chain of events in the GPCR?

A
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8
Q

What do second messengers do?

A
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9
Q

What are 4 examples of effectors in a GPCR?

A
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10
Q

What are examples of GPCR? (receptor)

A
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11
Q

What is the second messenger of adenylate cyclase effector?

A

cAMP

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12
Q

What is reaction of adenylate cyclase to camp?

A

ATP to CAMP + PPi

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13
Q

Can adenylate cyclase link inhibitory and stimulatory receptors?

A

Yes

regulated by Gs and Gi

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14
Q

What are the stimulating receptors adenylate cyclase?

A

Beta adrenergic

ACTH

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15
Q

What are the inhibitory receptors of adenylate cyclase?

A

Alpha 2 receptors

Muscarunic

Opiate

GABA b

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16
Q

What does camp activate?

17
Q

What does the inhibitory GPCR cause? (Gi, no cAMP)

A

M2, Ach R = Decreased HR

Alpha2:

Inhibitory neurotransmitter release

Contraction in smooth muscle

inhibition of insulin

18
Q

What is the effect of activating the inhibitory opioid GPCR? (no cAMP)

A

SEDATION…

19
Q

What are the sites if action of opioid analgesics?

A

Peripheral

Spinal

Supraspinal (medulla, thalamus, cortex)

20
Q

What is the best known opioid anagesic?

21
Q

What is the most commonly prescribed opioid analgesic?

22
Q

What are naturally occurring opioids?

A

Endorphins

23
Q

What are compounds related to opioids?

A

Methadone

Dimorphine (heroine)

Fentanyl

24
Q

What G protein activates PLC?

25
What are the second messenger of PLC?
IP3 DAG
26
What is the pathway of PLC (effector) in the GPCR?
27
What can GPCR also be called?
metabotropic receptors
28
What are the second messengers of PLC?
IP3 DAG
29
What activates the Gi (regulates adenylate cyclases)?
opioid agonists
30
What does increased cAMP in the cell cause? (activate PKA)
31
What are the contradictory effects of giving someone adrenaline?
Beta2 receptor increases glycogen and fat metabolism in liver, fat and muscle cells Beta1 receptor increases activity of voltage activated calcium channels in heart cells
32
Opioids inhibit AC and there for decreased cAMP and PKA levels, what is the effect of this?
PKA does not phosphorylate K+ channel or Ca2+ channel this open the K+ and closes the Ca2+ hyperpolarisation inhibition of AP
33
What receptor do opioid analgesics use?
mu receptors mainly for analgesic effects 3 types: mu, kappa, delta
34
What type of effector is PLC?
membrane bound enzyme
35
What does IP3 do? (PLC pathway)
increase in intracellular Ca2+
36
What does DAG do? (PLC pathway)
activation of PKC
37
IP3 increases Ca2+ in the cell, what does this result in?
38
DAG activates PKC, what does this result in?